3562-69-4Relevant academic research and scientific papers
Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands
Takahashi, Hidenori,Bekkali, Younes,Capolino, Alison J.,Gilmore, Thomas,Goldrick, Susan E.,Nelson, Richard M.,Terenzio, Donna,Wang, Ji,Zuvela-Jelaska, Ljiljana,Proudfoot, John,Nabozny, Gerald,Thomson, David
, p. 1549 - 1552 (2007/10/03)
We report the discovery of a novel class of glucocorticoid receptor (GR) ligands based on 1,2-dihydroquinoline molecular scaffold. The compounds exhibit good GR binding affinity and selectivity profile against other nuclear hormone receptors.
Compounds for the treatment of pain
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, (2008/06/13)
This invention provides methods of treating pain, urinary incontinence and other abnormalities mediated by a NPFF receptor, which comprises administering to a subject a therapeutically effective amount of a chemical compound which acts at the NPFF1 receptor, the NPFF2 receptor, or at both the NPFF1 and NPFF2 receptors.
Guanidines which are agonist/antagonist ligands for neuropeptide FF (NPFF) receptors
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, (2008/06/13)
This invention provides compounds having the structure: wherein X=CH, C(CH3) or N; each of R1, R2, R3, R4 and R5 is independently H, C1-C10 straight chained or branched alkyl, C2-C10 straight chained or branched alkenyl, C2-C10 straight chained or branched alkynyl, C3-C10 cycloalkyl, substituted or unsubstituted aryl, hydroxy, halogenated ether, nitro, amino, halogen, —CN, —C(═Z)R6, —C(═Z)OR6, —C(═Z)N(R6)2, —N(R6)—C(═Z)R6, —N(R6)—C(═Z)N(R6)2, —OC(═Z)R6, —C(═Z)OR6—OR6 or —SR6; wherein Z is O or S; and wherein R6 is C1-C10 straight chained or branched alkyl, aryl, (CH2)nQ, C2-C10 alkenyl, C3-C10 cycloalkyl, C5-C10 cycloalkenyl, wherein Q is OR7, SR7, N(R7)2 or aryl, wherein R7 is H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, wherein R2 and R3 and the carbons to which they are attached form a fused aryl, heteroaryl, C5-C10 cyclic alkyl or heterocyclic alkyl ring; or wherein R3 and R4 and the carbons to which they are attached form a fused aryl, heteroaryl, cyclic alkyl or heterocyclic alkyl ring; and wherein each alkyl, alkenyl, alkynyl and alkoxy group is optionally substituted with a substituent independently selected from Ra, where Ra is 1) hydroxy, 2) C1-C10 alkoxy, 3) halogen, 4) nitro, 5) amino, 6) CF3, or 7) carboxy, and each cycloalkyl group is optionally substituted with a substituent independently selected from Rb, where Rb is 1) a group selected from Ra, 2) C1-C7 alkyl, 3) C2-C7 alkenyl, 4) C2-C7 alkynyl or 5) cyclic C1-C10 alkyl, and each aryl is optionally substituted with R1. This invention also provides methods of treating pain, urge incontinence; as well as methods of preparing the compounds.
Novel facile synthesis of 2,2,4 substituted 1,2-dihydroquinolines via a modified Skraup reaction
Theoclitou, Maria-Elena,Robinson, Leslie A.
, p. 3907 - 3910 (2007/10/03)
A variety of 2,2,4 substituted 1,2-dihydroquinolines were synthesized from substituted anilines or aminoheterocycles and the corresponding ketones in good yield via the use of lanthanide catalysts and microwave technology. This method can be readily applied to the general synthesis of combinatorial libraries of dihydroquinolines.
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore
Pooley, Charlotte L. F.,Edwards, James P.,Goldman, Mark E.,Wang, Ming-Wei,Marschke, Keith B.,Crombie, Diane L.,Jones, Todd K.
, p. 3461 - 3466 (2007/10/03)
A series of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines was synthesized and tested for functional activity on the human progesterone receptor isoform B (hPR-B) in mammalian (CV-1) cells. The lead compound LG001447 (1,2-dihydro- 2,2,4-trimethyl-6-phenylqu
